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柚皮化学成分及其生物活性的研究

Studies on the Chemical Constituents of the Pericarps of Citrus Grandis(L.) Osbeck and Its Pharmacological Activities

【作者】 刘丽春

【导师】 李平亚;

【作者基本信息】 吉林大学 , 制药工程, 2012, 硕士

【摘要】 柚[Citrus grandis(L.) Osbeck]为芸香科柑橘属植物,其果实柚(pomelo,shaddock),又称柚子、文旦等;柚皮为柚类的干燥果皮,又名柚子皮、气柑皮、橙子皮等。中医认为,柚皮能化痰,消食,下气,快膈;主治气郁胸闷、脘腹冷痛、食滞、咳喘、疝气。现代医学研究表明:柚皮提取物具有抗氧化、降血脂、降血糖、抗菌、抗癌、止咳祛痰、抗炎镇痛等生物活性。我国柚类栽培历史悠久,资源丰富,品种繁多;近年来,柚类的生产面积和生产量持续上升,一些名优品种如沙田柚、琯溪蜜柚等已经形成大规模生产,并逐步打入国际市场;但绝大部分柚皮在柚类加工和食用后一般均废弃,造成了资源浪费和环境污染;为了更充分的利用柚皮资源,扩大柚果的利用途径,本论文对琯溪蜜柚果皮的化学成分和生物活性进行系统研究。首次对琯溪蜜柚果皮75%乙醇提取物的化学成分进行系统研究,利用分步萃取法和多步硅胶柱色谱,制备薄层色谱,半制备型HPLC,重结晶等手段分离得到14个单体化合物。通过理化性质分析及波谱(13C-NMR、~1H-NMR、HMBC等)解析,确定了其中10个化合物的结构,分别为:柚皮苷(1),柚皮素-4’-O-葡萄糖苷(2),葡萄内酯(3),7-羟基香豆素(4),柠檬苦素(5),木栓酮(6),邻苯二甲酸二甲酯(7),月桂酸(8),蔗糖(9),β-谷甾醇(10);其中化合物1~10均为首次从该种植物中分离得到。首次采用二甲苯致小鼠耳肿胀法和热板法,对柚皮提取物的抗炎镇痛活性进行研究,结果表明:与模型组相比,柚皮提取物中、高剂量组对于二甲苯引起的炎症反应均具有抗炎活性,且中剂量组与阳性药的抗炎活性相似;与空白组相比,柚皮提取物中、高剂量组在两小时内对热刺激引发的小鼠痛反应时间有明显的延长作用,且药效有良好的延续性。故柚皮提取物有一定的抗炎镇痛活性。

【Abstract】 The plant Citrus grandis(L.) Osbeck (Rutaceae) is commonly known as pomelo orbuntan,.ect. The pomelo peel is the dried peel of the pummelo. Traditional Chinesemedicine believes that pomelo peel can be used in dissipating phlegm, promoting digestionand stopping coughing,.ect. Modern medical research shows: its extract exhibits widelybiological activities such as antioxidant, hypolipidemic, hypoglycemic, antibacterial,anticancer, cough expectorant, anti-inflammatory and analgesic and so on.Pummelo cultivation in China has a long history, rich in resources, and more varieties.In recent years, Citrus production area and volume are continuely rising, and some of thefamous varieties such as shatianyou, Guanxi honey pomelo have formed a large-scaleproduction, and gradually entering the international market. But most of pomelo peel afterprocessing and consumption are generally abandoned, resulting in waste of resources andpollution of the environment. In order to find out more chemical constituents in pomelo peeland to develop more new healthy maintenances and drug products, I gave comprehensiveresearches. The research methods and results are as follows:Firstly, pomelo peel was extensively extracted with75%alcohol. The combinedextracts were concentrated in vacuo until no-alcohol. Then I got the total extracts, whichwere extracted further by petroleum ether, chloroform, acetic ether and n-butyl alcohol inturn. By using silica gel column chromatography, HPLC, TLC and re-crystallizing methods,fourteen compounds were obtained. Among of them, ten compounds structures wereidentified with the chemical and spectral evidences (13C-NMR,1H-NMR, HMBC). Theyare Naringin(1), Naringenin-4’-O-glucoside(2), Aurapten(3), Umbelliferone(4),Limonin(5),Friedelin(6), Dimethyl phthalate(7), Lauric acid(8), Sucrose(9), β-Sitosterol(10).Compound1~10were first obtained from the pericarps of Guanxi honey pomelo.The anti-inflammatory and analgesic effect of pomelo peel extracts was observed on dimethyl benzene-induced auricular edema and hot plate test in mice. The results indicatedthat the medium and high dose of pomelo peel extracts, compared with model group, hadsignificant anti-inflammatory effects; and compared with the blank group, both of themsignificantly prolonged the time of pain reaction in mice within two hours, and efficacyhave good continuity. So pomelo has certain anti-inflammatory and analgesic effect inanimal models.

  • 【网络出版投稿人】 吉林大学
  • 【网络出版年期】2012年 10期
  • 【分类号】R284.1;R285
  • 【被引频次】3
  • 【下载频次】701
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